PT  - JOURNAL ARTICLE
AU  - C. J. Daly
AU  - C. M. Milligan
AU  - G. Milligan
AU  - J. F. Mackenzie
AU  - J. C. Mcgrath
TI  - Cellular Localization and Pharmacological Characterization of Functioning <em>Alpha</em>-1 Adrenoceptors by Fluorescent Ligand Binding and Image Analysis Reveals Identical Binding Properties of Clustered and Diffuse Populations of Receptors
DP  - 1998 Aug 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 984--990
VI  - 286
IP  - 2
4099  - http://jpet.aspetjournals.org/content/286/2/984.short
4100  - http://jpet.aspetjournals.org/content/286/2/984.full
SO  - J Pharmacol Exp Ther1998 Aug 01; 286
AB  - A fluorescent quinazoline derivative was shown to retain high affinity for, and act as a competitive antagonist at, alpha-1 adrenoceptors. This allowed it to be used in live cells to localize receptors and to quantify receptor binding characteristics. The technique was demonstrated and validated on fibrobasts transfected with a recombinant alpha-1d adrenoceptor. Using confocal laser scanning microscopy and image analysis methods both diffuse and clustered binding sites were found: their binding characteristics were assessed and found comparable to radioligand binding on membrane preparations. This approach should have widespread applicability in nonradioactive assays determining the location, quantity and binding properties of receptors and other biological molecules on live tissue. The American Society for Pharmacology and Experimental Therapeutics